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PubMedDate not supplied

The hydrolysis activation of the doxorubicin cardioprotective agent ICRF-187 [+)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane).

ICRF-187 [(+)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane] has shown promise [Speyer et al., N. Engl. J. Med. 319, 745 (1988)] as a cardioprotective agent against what may be an iron-based doxorubicin (Adriamycin)-induced cardiotoxicity. ICRF-187 likely exerts its action through its rings-opened hydrolysis product, a compound that has an EDTA-type structure and, likewise, strongly binds metal ions. The hydrolysis of ICRF-187 was followed spectrophotometrically in the ultraviolet and was shown to be pseudo-first-order over a wide pH range. The hydrolysis mechanism was shown to have a hydroxide-catalyzed path and a pH-independent path similar to the hydrolysis of other imides. The anionic form of ICRF-187 (with a pKa of 9.6 at 37 degrees C) was resistant to hydroxide attack. The kinetically, spectroscopically and potentiometrically determined pKa values were all in excellent agreement and thus provided a test of the mechanism. Each imide group underwent hydrolysis and ionization independently of the other. The rate of ICRF-187 hydrolysis was also followed by observation of the removal of Cu2+ from a Cu2(+)-doxorubicin complex by the ICRF-187 hydrolysis product.

Chemical Phenomena↗
PubMed1990

Role of (+-)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane (ICRF-187) in modulating free radical scavenging enzymes in doxorubicin-induced cardiomyopathy.

This study was designed to investigate the mechanism by which (+-)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane (ICRF-187) protects against doxorubicin cardiotoxicity. Others have hypothesized that the major factor contributing to doxorubicin cardiotoxicity is the depletion of the antioxidant defense mechanisms of the heart induced by doxorubicin. Mice were acutely (24-h exposure) or chronically (13-week exposure) treated with doxorubicin to develop a model for cardiotoxicity. Five-week-old BALB/c mice were given i.p. injections of doxorubicin alone or 30 min after ICRF-187, while control mice received ICRF-187 or 0.9% NaCl solution alone without doxorubicin. Electron microscopy of the mouse hearts demonstrated conclusively that doxorubicin was cardiotoxic after 13 weeks of exposure, showing mitochondrial degeneration and disruption of the myofibrillar organization. Furthermore, normal morphology of the electron micrographs after treatment with doxorubicin and ICRF-187 indicated that ICRF-187 was cardioprotective. The activities of the antioxidants superoxide dismutase, glutathione peroxidase, and catalase and the concentration of reduced glutathione were measured in the heart, liver, kidneys, and skeletal muscle of mice treated with doxorubicin, ICRF-187, or the drug combination. After acute or chronic exposure to the drugs there was no significant difference in enzyme or reduced glutathione levels compared to the control mice in any of the treatment groups. It was concluded that neither the cardioprotective effect of ICRF-187 nor the cardiotoxicity induced by doxorubicin was related to an effect on cardiac antioxidants, but rather another mechanism operated in this particular model.

Animals↗
PubMed1990

Effects of propane-2, 2-diphosphonate (PDP) on matrix-induced ectopic bone formation in comparison to ethane-1-hydroxy-1, 1-diphosphonate (EHDP).

The most prominent effect of propane-2, 2-diphosphonate (PDP) and ethane-1-hydroxy-1, 1-diphosphonate (EHDP) on matrix-induced ectopic bone in the rat was a dose-dependent inhibition of osteogenesis in the early phases of development. The delay was seen as a consequence of osteoprogenitor cell inhibition. Additionally, later phases of bone maturation were disturbed by interference with the mineralization and remodeling processes. However, direct effects on the calcium phosphates of bone are only of minor additional value, which remains of lesser importance in comparison to the cellular impairment. After withdrawal of diphosphonates, the effects were nearly completely remitted. Neither PDP nor EHDP, even given in high doses, resulted in a lasting reduction in ectopic mass. The remission may be referred to the recovery of cell activities, whereas the mineral impregnation of osteoidosis was, if at all, of little importance. For treatment of ectopic osteogenesis PDP proved inefficient.

Animals↗
PubMed1990

[Antidotal effects of sulfhydryl compounds on acute poisonings by sodium ammonium dimethyl-2-(propane-1,3-dithiosulfate) monohydrate, nereistoxin and cartap].

Sodium dimercaptopropanesulphonate (DMPS) and sodium dimercaptosuccinate (DMS) were discovered to be effective antidotes for acute poisoning of insecticides SCD [sodium ammonium dimethyl-2-(propane-1,3-dithiosulfate) monohydrate], nereistoxin (4-N,N-dimethylamino-1,2-dithiolane) and cartap (dihydronereistoxin dicarbamate). In mice, DMPS (250 mg/kg) or DMS (1000 mg/kg) ip 20 min before SCD increased LD50 of ig SCD from 97 to 374 or 251 mg/kg, respectively. The prophylactic effect of DMPS was better than that of DMS. Administration of DMPS prior to cartap increased LD50 of ig cartap from 130 to 375 mg/kg. The therapeutic effect of DMPS was also demonstrated in SCD-poisoned conscious rabbits. DMPS 62.5 mg/kg or DMS 500 mg/kg iv completely antagonized the neuromuscular blockade and respiratory depression caused by SCD, nereistoxin and cartap in anesthetized rabbits. The antagonism of SCD-induced neuromuscular blockade by cysteine (400 mg/kg, iv) was less effective and of shorter duration than that by DMPS and DMS. Dimercaprol 50 mg/kg im showed little effect on SCD-induced paralysis. The antagonistic actions of sulfhydryl compounds on neuromuscular blockade induced by these insecticides probably belong to chemical antagonism.

Animals↗
PubMed1985

Comparison of the Arrhythmogenic Actions of (-)-Isoprenaline, Dobutamine and the selective beta 1-adrenoceptor agonist, (+/-)-(1-[3',4'-dihydroxyphenoxy] -2-hydroxy-[3",4"-dimethoxy phenethylamino]-propane)-oxalate (Ro 363).

In guinea-pig left atrial preparations, concentrations of (-)-isoprenaline and (+/-)-(1-[3',4'-dihydroxyphenoxy] -2-hydroxy-[3",4"-dimethoxyphenethylamino]-propane)-oxalate (Ro 363) causing maximal inotropic responses produced small reductions in effective refractory period. Dobutamine had little effect on the refractory period except at supramaximal inotropic concentrations, when increases in effective refractory period were produced. Isolated perfused heart preparations from guinea-pigs developed arrhythmic contractions following the administration of (-)-isoprenaline, Ro 363 and dobutamine in doses producing 70-100% of their maximal chronotropic responses. The arrhythmogenic activity of the three agonists paralleled their respective beta 1-receptor stimulant properties. In chloralose-anaesthetized cats, the 3 agonists, (-)-isoprenaline, Ro 363 and dobutamine, when compared to epinephrine (adrenaline), were essentially devoid of arrhythmogenic activity in animals in which cardiac sensitization was induced by 3-dimethylamino-2-methyl-2-phenoxypropiophenone hydrochloride (U-0882) or halothane. However, all 3 agonists elicited ventricular arrhythmias following the administration of subarrhythmic doses of ouabain and increased the number of subauricular escape beats which occurred during vagal nerve stimulation in non-ouabain treated animals. In all cases the arrhythmogenic activity of the drugs paralleled their relative activity for eliciting rises in heart rate.

Adrenergic beta-Agonists↗
PubMed1976

The antiarrhythmic and cardiovascular properties of 1-dimethyl isopropylamino-3-(2-phenylphenoxy)-propan-2-ol chloride, UM-424.

The quarternary ammonium compound, UM-424 [1-dimethyl isopropylamino-3-(2-phenylphenoxy)-propan-2-ol chloride], was evaluated for its antiarrhythmic and hemodynamic effects. UM-424 converted ouabain-induced ventricular tachycardia in the anesthetized dog when administered in an average dose of 4.6 mg/kg i.v. Pretreatment of anesthetized dogs with UM-424, 10 mg/kg, provided complete protection against the development of premature beats and ventricular fibrillation when the left anterior descending coronary artery was occluded for 20 minutes and then released. UM-424 was effective in reversing ventricular arrhythmias in conscious animals which had been subjected to a two-stage ligation of the anterior descending coronary artery. The mean ectopic rate in a group of five dogs was 143 +/- 4.0 (S.E.M.) beats/min 24 hours after coronary ligation. Normal sinus rhythm was restored with a mean dose of 9.5 mg/kg of UM-424 and was maintained for a period in excess of 60 minutes. The ventricular fibrillation threshold was increased from a control value of 4.0 +/- 0.4 to 26.2 +/- 8.6 mA (P less than .05) 30 minutes after pretreatment with UM-424, 10 mg/kg. Inotropic and chronotropic dose-response studies to isoproterenol in the anesthetized dog demonstrated that the quarternary compound lacked beta adrenergic receptor blocking properties. UM-424, 10 mg/kg, did not produce any persistent changes in spontaneous heart rate, cardiac contractile force, left ventricular dP/ct, mean arterial blood pressure, cardiac output and mean pulmonary arterial pressure.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

[Characteristics of the generation of transmembrane current higher harmonics in lipid bilayers in glycerol and 1,2-propane diol solutions].

It is shown that structural rearrangements of bilayer lipid membrane induced by glycerol and 1,2-propane diol result in noncompensated second harmonic of transmembrane current having quadratic dependence on input voltage and a weak dependence on frequency. The third harmonic has cubic dependence on input voltage and decreases with an increase in frequency. The mechanism is discussed according to which generation of non-compensated second harmonic is due to the formation of the intermediate lipid phase with viscoelastic properties differing from the initial bilayer in the process of structural rearrangements. The presence of this phase conditions the possibility of appearance of noncompensated second harmonic.

Electricity↗
PubMedDate not supplied

Determination of epimeric 1-(3-indolyl) propane -1,2,3-triol isolated from Balansia epichloe.

Investigations into diseases in cattle grazing on grass pastures infected with clavicipitaceous fungi have resulted in the isolation and characterization of erythro and threo 1-(3-indolyl) propane-1,2,3-triol from cultures of Balansia epichloë (Weese). Gas chromatography-mass spectroscopy analyses of synthetic and natural epimers as their trimethylsilyl derivatives is described. Toxicity studies with fertile chicken eggs demonstrated that the threo epimer was the more active compound. The ratio of erythro to threo was calculated at 3:2 in the natural isolate.

Animals↗
PubMed1980

[Pharmacological studies of 2-methyl-3(2-phenyl-3-methyl-tetrahydrooxazino)-propiophenone hydrochloride and 1-phenoxycarboxy-1-phenyl-2-methyl-3(2-phenyl-3-methyl-tetrahydrooxazino)-propane hydrochloride compounds].

The authors used the compounds 2-methyl-3)2-phenyl-3-methyl tetrahydroxasino)-propiophenone hydrochloriad (code PsI) and 1-phenoxycarboxy-1-phenyl-2-methyl-3 (2-phenyl-3-methyl-tetrahydroxasino-propan hydrochlorid(code P3) and carried out the following studies: influence of tripamine, corasol and strichnine seizures 1-phenoxycarboxy--1-phenyl-2-methyl--3 (2-phenyl--3-methyl-tetrahydroxasino) propar hydrochlor (Code P8) in white mice, effect on the hypertensive action of reserpine in white rats, investigations on the analeptic action in urethanized cats as well as on the analgetic effect, examined both by the test of "hot plate" and the method of Hendreshot-Forsaith. The examined compounds, administered in a dose of 1/6 of LD50, showed analgetic effect weaker than that of the preparations Morphinum hydrochloricum and Analigin, but their analeptic effect was less manifested that of of corasol. Similar to MAO-inhibitor-oproniazid although in smaller degree the compound PS1 potentiated tripamine seizures and inverted the hypotensive effect of Reserpine into hypertensive.

Analgesics↗
PubMed1983

Synthesis and pharmacological activity of some 1-alkylamino-3-(2'-methoxy-4'-diethylcarbamoyl-phenoxy)propan-2-ols.

The synthesis and pharmacological properties of some 1-alkylamino-3-(2'-methoxy-4'-diethylcarbamoylphenoxy)propan-2-ols, related to beta-adrenergic drugs, are described. The above compounds were found to possess beta 1 and beta 2-adrenolytic activity associated with local anesthetic and antiarrhythmic activities, which are clearly inferior to those of propranolol.

Adrenergic beta-Antagonists↗
PubMed1981

Effects of the L isomer (+)-1,2-bis(3,5-dioxopiperazine-1-yl)propane on cell survival and cell cycle progression of cultured mammalian cells.

The effects of the L isomer (+)-1,2-bis(3,5-dioxopiperazine-1-yl)propane (ICRF 159; NSC 169780) on cell viability, growth, and progression through the cell cycle were investigated in suspension cultures of murine leukemia (Friend leukemia and L1210) cells and normal human lymphocytes stimulated with phytohemagglutinin and in adherent cultures derived from human neuroblastoma and Chinese hamster ovary (CHO) cells. CHO cell colony formation was inhibited by 50% following either an 8.5-hr exposure of exponentially growing cells to 10 micrograms ICRF 159 per ml or a 24-hr exposure to 3 micrograms ICRF 159 per ml. This effect was cell cycle phase specific; early G1- and G2-phase cells were more sensitive than were late-G1- or early and mid-S-phase CHO cells. Stationary-phase CHO cells were unaffected by the drug at concentrations up to 500 micrograms/ml. Incubation of L1210 cells with 3 micrograms ICRF 159 per ml for 24 hr or with 10 micrograms ICRF 159 per ml for 6 hr inhibited cell growth by 50%. In contrast, 24-hr incubation of human lymphocytes with up to 50 micrograms ICRF 159 per ml had no effect on their viability or on their ability to be stimulated by phytohemagglutinin. Constant exposure of Friend leukemia, L1210, human neuroblastoma, and phytohemagglutinin-stimulated human lymphocytes to 10.0 to 50 micrograms ICRF 159 per ml resulted in inhibition of cell division which led to cell growth at higher ploidy levels. Thus, proliferating human cells of normal or tumor origin and murine leukemic cell lines all had a similar sensitivity to the drug. Detailed analysis of cell cycle progression in L1210 cells in the presence of the drug determined that cell progression through G1 phase (G1A to G1B transition) was slowed by approximately 50%. The rate of traverse of cells through S phase was also slowed. However, the most pronounced effect was the accumulation of cells in G2 phase occurring almost immediately after addition of the drug. The data suggest that the L isomer has a range of cytotoxicity and identical cytokinetic effects similar to that of the clinically tested racemate (+/-)-ICRF 159 (NSC 129943) and, therefore, that the more soluble L isomer may have increased clinical applicability.

Animals↗
PubMed1984

Effects of AVS (1,2-bis(nicotinamido)propane) on platelet function and vascular endothelium.

The effects of 1,2-bis(nicotinamido)propane (AVS) on platelet function and vascular endothelium were investigated using various experimental thrombosis and vascular endothelial injury models. Neither in vitro platelet aggregation induced by ADP, collagen or arachidonate nor ex vivo platelet aggregation by ADP or collagen could be antagonized by AVS. On the other hand, AVS prevented mice, rats and rabbits from death induced by acute cerebral or pulmonary thromboembolism following the injection of arachidonate or collagen. These activities were as potent as those of acetylsalicylic acid. The disrupting actions of citrate and/or lipidperoxide (13-hydroperoxy linoleic acid) on endothelium were well inhibited by the pretreatment of AVS. AVS did not inhibit cyclooxygenase, increased prostacyclin (PGI2)/thromboxane A2 (TXA2) ratio in the coupled system of platelets and aortic microsomes. In conclusion, AVS inhibited thrombus formation in vivo while it was ineffective in vitro platelet alone system, which may result from the actions of this agent on both platelets and vascular endothelium. The above-mentioned results clearly show that AVS may be a new potent anti-vascular damaging agent with both endothelium stabilizing and PGI2 enhancing activities.

Animals↗
PubMed1984

[Microbiologic study of a new disinfectant: decyloxy-3-hydroxy-2-amino-1-propane hydrochloride].

Decominol exhibits bactericidal activity in a concentration of 0.05% (NF T 72-151). This concentration is increased five-fold in the presence of an albumin-yeast extract mixture, and 2.5-fold in the presence of hard water (60 degrees French). At pH 5.0, 0.5% concentration is not bactericidal (NF T 72-171) Fungicidal activity (T 72-201) is weak at 20 degrees and 50 degrees C and the sporicidal tests (T 72-231) establish the lack of sporicidal activity at 10%. Decyloxy-3 hydroxy-2 in 0.2 amino-1 propane hydrochloride to 1.5% concentrations used in a meat-canning factory ensures satisfactory disinfection of correctly cleansed surfaces. It also proves useful for sterilization of circuits where it can be used as an adjunct to the lethal action of heat.

Bacteria↗
PubMed1982

A pharmacological study of propane-1,2-diol.

Propane-1,2-diol (propylene glycol, PG), considered to be a safe solvent and commonly used as a vehicle in pharmacological and toxicological investigations, showed various neuropsychopharmacological activity in albino mice and rats. In lower concentrations (10-20%), at dose level of 10 ml/kg, PG did not show any significant neuropsychopharmacological activity either by i.p. or p.o. routes. But higher concentrations (50-100%), at same dose level by i.p. route, were found to have moderate to marked effect. There was decrease in locomotor activity, body and limb tone, respiration, rectal temperature and suppression of secondary conditioned responses. Significant potentiation of pentobarbitone (pentobarbital) hypnosis, slight increase in d-amphetamine toxicity in aggregated mice and pronounced analgesic and anti-inflammatory activity were also observed. Most of the above effects were also observed on p.o. treatment but the effects were of lesser degree. PG did not produce any effect on dog or cat blood pressure up to 100% concentration at the dose level 0.5 ml/kg. However, it potentiated the adrenaline (epinephrine) and noradrenaline (norepinephrine) response. On isolated smooth muscle preparations, in 50-100% concentrations, a dose-dependent non-specific blockade was observed against agonists viz. acetylcholine, histamine, 5-HT and barium chloride. No effect was seen on cardiac tissue preparation. On the basis of present findings, it is suggested that propylene glycol as a solvent be used only in low concentration of not more than 10% for pharmacological and toxicological investigations.

Analgesics↗
PubMed1982

Inhibition of the R3327MAT-Lu prostatic tumor by diethylstilbestrol and 1,2-bis(3,5-dioxopiperazin-1-yl)propane.

We have previously described the inhibitory effects of diethylstilbestrol on the growth of the androgen-independent, anaplastic Copenhagen rat prostatic tumor, R3327AT, which has a low metastatic potential. We have now selected a variant of the R3327AT tumor that metastasizes exclusively to the lungs, and we have designated it the R3327MAT-Lu. In a dose-response protocol, diethylstilbestrol was inhibitory to the primary R3327MAT-Lu tumor, thereby also inhibiting the formation of lung metastases. Inhibition was also observed in this model tumor by the chemotherapeutic agent 1,2-bis(3,5-dioxopiperazin-1-yl)propane.

Animals↗
PubMed1994

A structure activity relationship study on 1-isopropylamino-3-(2'-substituted naphthoxy)-propan-2-ois analogs.

The structure activity relationship of 1-isopropylamino-3-(2'-substituted naphthoxy) propan-2-ois analogs, which are beta-adrenergic blocking drugs, is discussed. The blocking activity of these compounds is found to be dominantly controlled by electronic and steric factors. Significant correlations have been obtained between the blocking activity and negentropy, equalized eletronegativity and partial charge.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

Disposition of a new antiinfective agent 1,3-di(4-imidazolino-2-methoxyphenoxy)propane in male rats.

The disposition of 1,3-di[4-imidazolino-2-methoxyphenoxy]propane (DMP) is described in male rats following a single 2.5 mg/kg intravenous or 10 mg/kg oral administration of DMP lactate in an aqueous (5% dextrose) solution. Following the intravenous administration, plasma concentrations of DMP declined in an apparent biexponential manner and were nonmeasurable after 24 hr. The mean terminal plasma elimination half-life was 14.9 hr. A volume of distribution of 18.7 liters/kg and a body clearance of 14.5 ml/min/kg were estimated. After oral administration, mean plasma concentrations of DMP reached a maximum of 39.6 ng/ml at 15 min and were nonmeasurable after 4 hr. The areas under the curve (AUC)0-24 of DMP was 2276 ng.hr/ml following the intravenous dose. The AUC0-4 was 68 ng.hr/ml following the oral dose. The AUC0-4 was 68 ng.hr/ml following the oral dose. Based on a comparison of AUC0-4, the oral bioavailability was 0.9%. A mean of 41.7 and 0.4% of the dose was excreted in urine as DMP following intravenous and oral administration, respectively. The tissue distribution and mass balance of total 14C were determined following a single 2.5 mg/kg intravenous administration of [14C]DMP.lactate. The concentrations of total 14C in all tissues were highest at 0.5 hr and declined with time thereafter. The highest concentration of 14C was in the kidneys, whereas the highest total amount was in the liver.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗